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    Pyrrolo[1,2-b] pyridazine derivatives having sPLA2 inhibitory effect
    1.
    发明授权
    Pyrrolo[1,2-b] pyridazine derivatives having sPLA2 inhibitory effect 失效
    具有sPLA2抑制作用的吡咯并[1,2-b]哒嗪衍生物

    公开(公告)号：US06472389B1

    公开(公告)日：2002-10-29

    申请号：US09673413

    申请日：2000-10-18

    申请人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Yoshikazu Fukui ,  Makoto Adachi

    发明人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Yoshikazu Fukui ,  Makoto Adachi

    IPC分类号： A61K315025

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is —(L1)—R6 wherein L1 is a divalent linking group of 1 to 18 atoms or the like, and R6 is a carbocyclic ring substituted by at least one non-interfering substituent or the like; R2 is C1 to C3 alkyl or the like; R3 is —(L2)-(acidic group); R4 and R5 are hydrogen atoms, non-interfering substituents, carbocyclic groups or the like; X is independently oxygen atom of sulfur atom; and RA is —C(═X)—C(═X)—NH2 or the like; the prodrugs thereof, their pharmaceutically acceptable salts, or their solvates, and a composition for inhibiting sPLA2 containing them as effective ingredients.

    摘要翻译： 本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中R1为 - （L1）-R6，其中L1为1至18个原子的二价连接基团等，R6为 被至少一个非干扰取代基等取代的碳环; R2是C1-C3烷基等; R3是 - （L2） - （酸性基团）; R4和R5是氢原子，非干扰取代基，碳环基团等; X独立地是硫原子的氧原子; RA为-C（= X）-C（= X）-NH 2等; 其前体药物，其药学上可接受的盐或其溶剂合物，以及用于抑制含有它们作为有效成分的sPLA2的组合物。

    Tricyclic compounds having sPLA2-inhibitory activities
    2.
    发明授权
    Tricyclic compounds having sPLA2-inhibitory activities 失效
    具有sPLA2抑制活性的三环化合物

    公开(公告)号：US06673781B1

    公开(公告)日：2004-01-06

    申请号：US10048348

    申请日：2002-02-01

    申请人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Tetsuo Okada ,  Makoto Adachi ,  Tomoyuki Ogawa

    发明人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Tetsuo Okada ,  Makoto Adachi ,  Tomoyuki Ogawa

    IPC分类号： C07D47104

    CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D491/14

    摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

    摘要翻译： 本发明提供具有sPLA2抑制活性的化合物。 由式（I）表示的化合物：其中R 1为（a）C 1至C 20烷基，C 2至C 20烯基，C 2至C 20炔基，碳环基，杂环基等; R 2是CONH 2或CONHNH 2; R 3和R 4之一是 - （L 2） - （酸性基团）其中L 2是与酸基连接的基团和连接基团的长度为1至5个原子，以及 另一个是氢原子; 其前体药物，其药学上可接受的盐或溶剂化物。

    Tricyclic compounds having sPLA2-inhibitory activities
    3.
    发明授权
    Tricyclic compounds having sPLA2-inhibitory activities 失效
    具有sPLA2抑制活性的三环化合物

    公开(公告)号：US06703385B1

    公开(公告)日：2004-03-09

    申请号：US10031443

    申请日：2002-01-22

    申请人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Makoto Adachi ,  Tomoyuki Ogawa

    发明人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Makoto Adachi ,  Tomoyuki Ogawa

    IPC分类号： A61K3133

    CPC分类号： C07D471/04

    摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is COCONH2 or the like; Q1 is a nitrogen atom or C—R4; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; R21 and R22 are hydrogen atoms or the like; X is —CR23R24— or the like wherein R23 and R24 are hydrogen atoms or the like; Y is —CR25R26— or the like wherein R25 and R26 are hydrogen atoms or the like; Z is CH2 or the like; a broken line ( - - - ) represents the presence or absence of a bond, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

    摘要翻译： 本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中R 1为（a）C 1至C 20烷基，C 2至C 20烯基，C 2至C 20炔基，碳环基，杂环基 或类似物; R 2是COCONH 2等; Q 1是氮原子或C-R 4; R 3和R 4之一是 - （L 2） - （酸性基团）其中L 2是与酸基连接的基团和连接基团的长度为1至5个原子，以及 另一个是氢原子; R 21和R 22是氢原子等; X是-CR 23 R 24 - 等，其中R 23和R 24是氢原子等; Y是-CR 25 R 26 - 等，其中R 25和R 26是氢原子等; Z是CH 2等; 虚线（ - - - ）表示键的存在或不存在，其前体药物，其药学上可接受的盐或溶剂合物。

    Process of producing ether-type thio-phospholipids
    5.
    发明授权
    Process of producing ether-type thio-phospholipids 失效
    生产醚型硫代磷脂的方法

    公开(公告)号：US5760270A

    公开(公告)日：1998-06-02

    申请号：US847771

    申请日：1997-04-23

    申请人： Mitsuaki Ohtani ,  Masahiro Fuji

    发明人： Mitsuaki Ohtani ,  Masahiro Fuji

    IPC分类号： C07C327/20 ,  C07C323/12 ,  C07C327/06 ,  C07C327/28 ,  C07F9/10 ,  C07F9/117

    CPC分类号： C07C327/28 ,  C07C323/12 ,  C07C327/06 ,  C07F9/10 ,  C07F9/117 ,  Y02P20/55

    摘要： A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17; A is C.sub.14 -C.sub.20 acyl group; G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

    摘要翻译： 制备式（I）的醚型硫代磷脂的方法：其中：n为13〜17的整数; A为C 14 -C 20酰基; G是选自以下的基团：作为细胞溶质磷脂酶A2抑制剂的合成底物有用的 ，所述方法适用于批量生产化合物（I），其中间体及其制备方法 同样提供。

    Pyrrolo[1,2-a]pyrazine spla2 inhibitor
    6.
    发明授权
    Pyrrolo[1,2-a]pyrazine spla2 inhibitor 失效
    吡咯并[1,2-a]吡嗪spl2抑制剂

    公开(公告)号：US06407104B1

    公开(公告)日：2002-06-18

    申请号：US09623591

    申请日：2000-09-05

    申请人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Tetsuo Okada

    发明人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Tetsuo Okada

    IPC分类号： A61K31519

    CPC分类号： A61K31/495 ,  C07D487/04

    摘要： wherein R1 is —(L1)—R6 wherein L1 is a divalent linking group of 1 to 18 atoms or the like, and R6 is a carbocyclic ring substituted by at least one non-interfering substituent or the like; R2 is C1 to C3 alkyl, C3 to C4 cycloalkyl or the like group; R3 is —(L2)-(acidic group); R4 and R5 are hydrogen atoms, non-interfering substituents, carbocyclic groups or the like; RA is —C(═X)—C(═X)—NH2 or the like; and X is independently oxygen atom or sulfur atom; the prodrugs thereof, their pharmaceutically acceptable salts, or their solvates, and a composition for inhibiting sPLA2 containing them as effective ingredients.

    摘要翻译： 其中R1为 - （L1）-R6，其中L1为1至18个原子等的二价连接基团，R6为被至少一个非干扰取代基等取代的碳环; R2是C1-C3烷基，C3-C4环烷基等基团; R3是 - （L2） - （酸性基团）; R4和R5是氢原子，非干扰取代基，碳环基团等; RA是-C（= X）-C（= X）-NH 2等; X独立地为氧原子或硫原子; 其前体药物，其药学上可接受的盐或其溶剂合物，以及用于抑制含有它们作为有效成分的sPLA2的组合物。

    Pyrrolotriazine derivatives having spla2-inhibitory activities
    8.
    发明授权
    Pyrrolotriazine derivatives having spla2-inhibitory activities 失效
    具有spl2抑制活性的吡咯并三嗪衍生物

    公开(公告)号：US06787545B1

    公开(公告)日：2004-09-07

    申请号：US10049912

    申请日：2002-02-20

    申请人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Tomoyuki Ogawa

    发明人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Tomoyuki Ogawa

    IPC分类号： C07D48704

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is a hydrogen atom or a group containing 1 to 4 non-hydrogen atoms; RA is —COCONH2 or the like; R3 is -(L2)-(acidic group) wherein L2 is a group connecting with an acid group; R4 is a hydrogen atom or the like, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

    摘要翻译： 本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中R 1为C 1至C 20烷基，C 2至C 20烯基，C 2至C 20炔基，碳环基，杂环基等 ; R 2是氢原子或含有1至4个非氢原子的基团; R A是-COCONH 2等; R 3是 - （L 2） - （酸性基团），其中L 2是与酸基连接的基团; R 4是氢原子等，其前药，其药学上可接受的盐或溶剂合物。

    Tricyclic azaindolizine derivatives having an sPLA2-inhibitory activities
    9.
    发明授权
    Tricyclic azaindolizine derivatives having an sPLA2-inhibitory activities 失效
    具有sPLA2抑制活性的三环唑烷衍生物

    公开(公告)号：US06756376B1

    公开(公告)日：2004-06-29

    申请号：US10129658

    申请日：2002-05-09

    申请人： Masahiro Fuji ,  Tetsuo Okada ,  Makoto Adachi

    发明人： Masahiro Fuji ,  Tetsuo Okada ,  Makoto Adachi

    IPC分类号： C07D48704

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein E is N or C—R4; G is N or C—R25; R1 is a carbocyclic group, heterocyclic group or the like; one of R3 and R4 is —(L2)-(acidic group), the other is a hydrogen atom, wherein L2 is a group connecting with an acid group; A ring is optionally substituted 5-8 membered cyclohexane ring or cyclohexene ring; R24 and R25 are a hydrogen atom or the like, its prodrug, their pharmaceutically acceptable salt, or hydrate thereof.

    摘要翻译： 本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中E为N或C-R 4; G是N或C-R 25; R 1是碳环基，杂环基等; R 3和R 4中的一个是 - （L 2） - （酸性基团），另一个是氢原子，其中L 2是与酸基连接的基团; 环是任选取代的5-8元环己烷环或环己烯环; R 24和R 25是氢原子等，其前药，其药学上可接受的盐或水合物。